巻号一覧
41 巻, 9 号
選択された号の論文の40件中1～40を表示しています
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木下 敏夫, 渡辺 幸弘, 高石 ゆみ子, 奥中 智子, 中尾 世津子, 古川 淳1993 年 41 巻 9 号 p. 1485-1490
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーSeveral new tricyclic hetero compounds possessing a pyrimidine ring were formed by reaction of 5-bromo- (and 5-nitro)-1-(2-bromoethyl, 3-bromopropyl, and 2-bromopropyl)-6-bromomethyl-3-methyl-2, 4(1H, 3H)-pyrimidinediones (1a-c and 7a, b) with thiourea derivatives : namely, 5-bromo-(and-5-nitro)-9-imino-3-methyl-(and 3, 11-dimethyl)-2, 4-dioxo-8, 1, 3, 10-thiatriazatricyclo[4.3.0.06, 10]dodecanes (2a-4a, 2c, and 8a-10a) and 5-bromo-(and 5-nitro)-9-imino-3-methyl-2, 4-dioxo-8, 1, 3, 10-thiatriazatricyclo[4.4.0.06, 10]tridecanes (2b-4b and 8b-10b). A new ring transformation reaction was found : compound 8b was converted to 7-acetylimino-3-methyl-2, 4-dioxo-6, 1, 3, 8-thiatriazatricyclo-[4.4.0.15, 8]dodec-5(12)-ene (11) by reaction with acetic anhydride.抄録全体を表示PDF形式でダウンロード (853K) -
崔 承彬, 手塚 康弘, 山下 浩子, 菊池 徹, 中野 洋文, 玉沖 達也, 朴 鐘喜1993 年 41 巻 9 号 p. 1491-1497
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA new tetrameric proanthocyanidin named davallin (1) and two new phenolic glycosides, 5-O-β-D-(6-O-vanilloylglucopyranosyl)gentisic acid (6) and 4-O-β-D-(6-O-vanilloylglucopyranosyl)vanillic acid (7), have been isolated from the rhizomes of Davallia mariesii MOORE together with six known compounds, procyanidin B-2 (2) and B-5 (3), epicatechin-(4β→8)-epicatechin-(4β→6)-epicatechin (4), epicatechin-(4β→6)-epicatechin-(4β→8)-epicatechin-(4β→6)-epicatechin (5), protocatechuic acid (8), and 1-naphthol-β-D-glucopyranoside (9). Structures of the three new compounds (1, 6, and 7) were determined by means of spectroscopic methods including two-dimensional NMR techniques.Among the compounds obtained, 1 and 2 inhibited protein kinase C with IC50 values of 3.5 and 8.6 μM, respectively.抄録全体を表示PDF形式でダウンロード (894K) -
廣橋 満, 木戸 勝, 山本 栄仁, 小島 裕, 實川 浩一郎, 藤井 節郎1993 年 41 巻 9 号 p. 1498-1506
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーThe reactivities of 5-fluorouracil (5-FUra) degradation inhibitors, 2, 4- (2) and 2, 6-dihydroxypyridines (3), were investigated. Acylation of 2 and 2, 4-bis(trimethylsilyloxy)pyridines with equimolar amounts of acid chlorides preferentially occurred at the 4-OH and 2-OH positions, respectively, and the structure of monobenzoylated 5-chloro-2, 4-dihydroxypyridine (2b) was determined as 4-benzoyloxy-5-chloro-2-pyridone (5b) by X-ray crystallo-graphic analysis. Compounds 2 and 3, as well as the N-2-tetrahydrofuryl (11), N-alkyl (12), and N-carbamoyl (14) derivatives of 2, exhibit dynamic keto-enol tautomerism. The acyl derivatives of these pyridines are labile and are thought to be active esters. Monoacyl ester derivatives of these pyridines were combined with 5-FUra analogs to develop novel antitumor agents containing an inhibitor of 5-FUra degradation. One of them, 3-[3-(6-benzoyloxy-3-cyano-2-pyridyloxycarbonyl)benzoyl]-1-ethoxymethyl-5-fluorouracil (BOF-A2) (22b), was the most effective and is currently undergoing late phase-II clinical trials.抄録全体を表示PDF形式でダウンロード (1122K) -
郭 悦雄, 林 生財1993 年 41 巻 9 号 p. 1507-1512
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーOxidation of 1-arylprop-1-enes by using the reagent system CrO3-HClO4-CH3CN at 0-5°C gave seven products from methyl isoeugenol, five from ethyl isoeugenol, four from benzyl isoeugenol, and five from isosafrole. Cagayanone was obtained from isosafrole in one step. The structures of the products were elucidated and the mechanism of their formation is discussed.抄録全体を表示PDF形式でダウンロード (863K) -
葛西 浩一, 岡田 清, 山次 信幸1993 年 41 巻 9 号 p. 1513-1520
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーSixteen novel 6'-O-substituted 2', 7'-dichlorofluorescein N-acetyl-β-D-glucosaminides (2a-p) were synthesized from 2', 7'-dichlorofluorescein 2, 3, 4, 6-tetraacetyl-β-D-glucosaminide (10), prepared through 3 steps from 2', 7'-dichlorofluorescein (3). These N-acetyl-β-D-glucosaminides were examined to evaluate their solubility under the weakly acidic rate-assay conditions (pH 5.0) and their kinetic parameters with N-acetyl-β-D-glucosaminidase. Among these compounds, 6'-O-carboxymethyl- (2a), 6'-O-(N, N-dimethylaminoethyl)- (2i), and 6'-O-sulfoxyethyl-2', 7'-dichlorofluorescein N-acetyl-β-D-glucosaminides (2p), are considered to be potential chromogenic substrates for the rate-assay of N-acetyl-β-D-glucosaminidase, since they showed good solubility of more than 10mM, moderate Km values of 1.46-2.04mM, and higher sensitivity to the enzyme than 2-chloro-4-nitrophenyl-N-acetyl-β-D-glucosaminide.抄録全体を表示PDF形式でダウンロード (1216K) -
井上 博純, 松木 健司, 大石 篤郎1993 年 41 巻 9 号 p. 1521-1523
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーEnantioselective synthesis of (2R, 3S)-3-(4-methoxyphenyl)glycidic ester ((2R, 3S)-1) via the enzymatic hydrolysis of erythro-N-acetyl-β-(4-methoxyphenyl)serine (9) was investigated. Treatment of the obtained α-amino acid (-)-10 with NaNO2-KBr-dilute H2SO4, esterification, and subsequent oxiran-ring closure of the halohydrin gave the target compound (2R, 3S)-1 with high enantiomeric excess (94% ee).抄録全体を表示PDF形式でダウンロード (592K) -
清水 猛, 平沼 佐代子, 大久保 尊弘, 吉岡 宏輔1993 年 41 巻 9 号 p. 1524-1529
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーNovel hydrophenanthrene lactams (4a, b and 13-16) and hydrophenanthrene derivatives (5a-c and 6a-d) bearing an angular carboxymethyl group were synthesized in good yield via the tricyclic compounds (3a, b) readily prepared from the cyanomethyl derivative (2) of Wieland-Miescher ketone and 1-chloro-3-pentanone.抄録全体を表示PDF形式でダウンロード (899K) -
竹村 優子, 中田 裕美子, 東 美希, 十一 元晴, 岡野 正義, 深宮 斉彦, 大村 三男, 井藤 千裕, 中川 紀代美, 古川 宏1993 年 41 巻 9 号 p. 1530-1533
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーFive new pyranocoumarins, named cis-5-methoxydecursidinol (1), trans-5-methoxydecursidinol (2), cis-hassanin (4), trans-hassanin (5), and hassanidin (7), were isolated from the roots of some Citrus plants and their structures were elucidated by spectroscopic methods and chemical derivation from known coumarins.抄録全体を表示PDF形式でダウンロード (683K) -
渋谷 博孝, 黒須 三千夫, 皆川 和之, 片山 精司, 北川 勲1993 年 41 巻 9 号 p. 1534-1544
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーFor examination of the structure-activity relationship five analogues [(2'R)-2'-hydroxypalmitoyl (3), palmitoyl (4), (2'S)-2'-hydroxypalmitoyl (5), β-D-galactosyl (6), and 8, 9-dihydro (7) relevancies] of soya-cerebroside II (2), which is a calcium ionophoretic sphingoglycolipid isolated from soybean, have been synthesized by using our previously reported synthetic method for sphingoglycolipids. Examinations by using a W-08 (liquid-membrane type) apparatus and by means of the human erythrocyte membrane method, have shown that the (2'R)-2'-hydroxypalmitoyl analogue (3) exhibits higher ion-binding and ion-permeation activities for calcium ion than soya-cerebroside II (2), which contains 3 as the major component. It has also been found that the other analogues(5, 6, 7, 8) do not show those ionophoretic activities.An enantiomer (8) of the (2'R)-2'-hydroxypalmitoyl analogue (3) has been synthesized and its calcium ionophoretic activity examined. Compound 8 exhibits calcium ion-binding activity equal to that of 3, but 8 lacks the ability to support calcium ion-permeation through human erythrocyte membrane. Thus, human erythrocyte membrane precisely distinguishes the absolute configurations of 3 and 8 as regards calcium ionophoretic activity.抄録全体を表示PDF形式でダウンロード (1540K) -
森本 隆司, 村上 啓寿, 永津 明人, 榊原 仁作1993 年 41 巻 9 号 p. 1545-1548
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーTwo new sulfoquinovosyl diacylglycerols (SQDGs, 1, 2) one of which contained a branched fatty acid as an acyl substituent were isolated from the green alga Chlorella vulgaris, along with three known SQDGs (3-5). Their structures were determined on the basis of physicochemical evidence and enzymatic hydrolysis using lipase (from Rhizopus arrhizus).抄録全体を表示PDF形式でダウンロード (739K) -
麻生 真理子, 兼松 顯1993 年 41 巻 9 号 p. 1549-1556
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーSynthesis of cycloshikonin via successive Michael reaction-sigmatropic rearrangement of naphthodiquinone with O-silylated ketene acetals is described. The structure dependence of the reactivity of the side chain of intermediary naphthazarin derivatives has also been investigated.抄録全体を表示PDF形式でダウンロード (1276K) -
冨士 薫, 田中 圭, 宮本 寿1993 年 41 巻 9 号 p. 1557-1561
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーEnantioselective ethylation of benzaldehyde with diethylzinc in the presence of a catalytic amount of chiral piperazine derivatives was investigated. The chiral piperazine works as an asymmetric catalyst in the alkylation, yielding 1-phenylpropanol with a moderate enantioselectivity. The influence of structural variation of the piperazine ring upon the asymmetric induction and the mechanism involved are discussed.抄録全体を表示PDF形式でダウンロード (832K) -
長尾 常敦, 岩瀬 由紀子, 岡部 光1993 年 41 巻 9 号 p. 1562-1566
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーSix new echinocystic acid 3, 28-O-bisdesmosides, scaberosides Hc2, Hd, Hf, Hg, Hh and Hi, were isolated as their methyl esters from the ground part of Aster scaber THUNB. (Compositae), and their structures were determined based on spectral and chemical evidence as follows. Scaberoside Hc2 is 3-O-[O-β-D-xylopyranosyl-(1→3)-β-D-glucopyranosiduronic acid] echinocystic acid 28-{O-β-D-xylopyranosyl-(1→3)-O-β-D-xylopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl}ester, scaberoside Hd, 3-O-[O-β-D-xylopyranosyl-(1→3)-β-D-glucopyranosiduronic acid] echinocystic acid 28-{O-β-D-xylopyranosyl-(1→3)-O-β-D-xylopyranosyl-(1→3)-[O-β-D-xylopyranosyl-(1→4)]-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl} ester, scaberoside Hf, 3-O-[O-β-D-galactopyranosyl-(1→2)-β-D-glucopyranosiduronic acid] echinocystic acid 28-{O-β-D-xylopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl} ester, scaberoside Hg, 3-O-[O-β-D-galactopyranosyl-(1→2)-β-D-glucopyranosiduronic acid] echinocystic acid 28-{O-β-D-xylopyranosyl-(1→3)-O-β-D-xylopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl} ester, scaberoside Hh, 3-O-{O-β-D-galactopyranosyl-(1→2)-[O-β-D-xylopyranosyl-(1→3)]-β-D-glucopyranosiduronic acid} echinocystic acid 28-{O-β-D-xylopyranosyl-(1→3)-O-β-D-xylopyranosyl-(1→4)-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl} ester and scaberoside Hi, 3-O-[O-β-D-galactopyranosyl-(1→2)-β-D-glucopyranosiduronic acid] echinocystic acid 28-{O-β-D-xylopyranosyl-(1→3)-O-β-D-xylopyranosyl-(1→3)-[O-β-D-xylopyranosyl-(1→4)]-O-α-L-rhamnopyranosyl-(1→2)-[O-α-L-rhamnopyranosyl-(1→3)]-β-D-xylopyranosyl} ester.抄録全体を表示PDF形式でダウンロード (818K) -
北川 勲, 堀 一之, 内田 英美子, 陳 偉衆, 吉川 雅之, 任 家礼1993 年 41 巻 9 号 p. 1567-1572
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーFrom the air-dried roots of Glycyrrhiza uralensis FISCHER collected in Xinjiang province, China ("Shinkyo-Kanzo" in Japanese), a new oleanene-type triterpene oligoglycoside named licorice-saponin L3 and a new chalcone oligoglycoside named isoliquiritin apioside were isolated together with glycyrrhizin, 18α-glycyrrhizin, apioglycyrrhizin, arabo-glycyrrhizin, licorice-saponins A3, E2, G2, and H2, and six known flavonoid glycosides. On the basis of chemical and physicochemical evidence, the structures of licorice-saponin L3 and isoliquiritin apioside were elucidated as 3β-[α-L-rhamnopyranosyl(1→2)-α-L-arabinopyranosyl(1→2)-β-D-glucuronopyranosyloxy]-22β-acetoxy-24-hydroxyolean-12-en-30-oic acid (1) and 4-O-[β-D-apiofuranosyl(1→2)-β-D-glucopyranosyl]isoliquiritigenin (6), respectively.抄録全体を表示PDF形式でダウンロード (966K) -
執行 洋陸, 佐藤 精一, 渋谷 公幸, 高橋 良男, 山口 隆, 蘇木 宏之, 大田 富夫1993 年 41 巻 9 号 p. 1573-1582
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA series of disubstituted phenylpyridine derivatives was synthesized and their antiarrhythmic effects against chloroform-induced ventricular arrhythmias in mice were examined. Among them, 2- and 3-[2-(3-aminobutyramido)-4-(2, 2, 2-trifluoroethoxy)phenyl]pyridines (23h, 24h) and 3-[2-(3-aminobutyramido)-4-ethoxyphenyl]pyridine (24i) showed potent antiarrhythmic activity. They had approximately twice the potency of mexiletine (III). Compound 24i was selected from this series as a candidate for further development; it was found to have a class I B electrophysiological character and to show a slow kinetic rate-dependent block (RDB) of the sodium channel in cardiac muscle.抄録全体を表示PDF形式でダウンロード (1305K) -
新井 平八郎, 西岡 裕康, 丹羽 誠一, 山中 健史, 田中 芳明, 吉長 幸嗣, 小林 直美, 三浦 直良, 池田 勇五1993 年 41 巻 9 号 p. 1583-1588
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーBy chemical modification of a known prolyl endopeptidase (PEP) inhibitor (N-[N-(4-phenylbutanoyl)-L-prolyl]pyrrolidine; SUAM-1221), several arylalkanoyl derivatives (V-1-27) were synthesized and tested for in vitro inhibitory activity towards PEP from canine brain. Among them, 4-(2-thienyl)butanoyl derivatives (V-24-27) showed more potent PEP-inhibitory activity than SUAM-1221. The structure-activity relationships of these compounds are discussed.抄録全体を表示PDF形式でダウンロード (833K) -
重永 信次, 真鍋 孝司, 松田 博, 藤井 隆, 広井 純, 松尾 昌昭1993 年 41 巻 9 号 p. 1589-1595
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA number of N-[4-[4-(1H-indol-3-yl)piperidinoalkyl]-2-thiazolyl]alkanesulfonamides (8-21) were synthesized and evaluated for their preventive effects on systemic anaphylaxis in guinea pigs. Structure-activity analysis revealed that methane- and ethanesulfonamide derivatives having a one to three methylene tether between the piperidine and thiazole rings exhibited potent activity but the introduction of a substituent on the indole part reduced the activity. Administration (100mg/kg p.o.) of the four compounds 8, 9, 12, 13, together with ketotifen, oxatomide, terfenadine and azelastine as reference compounds, to mice revealed that only compound 8 caused no significant increase of the sleeping time induced by hexobarbital. In addition, compound 8 (10mg/kg i.v.) did not change the electroencephalogram in conscious rabbits. These results led to the selection of N-[4-[4-(1H-indol-3-yl)piperidinomethyl]-2-thiazolyl]methanesulfonamide (8, FK613) for further development as a novel antiallergic agent. Clinical evaluation of FK613 is now in progress.抄録全体を表示PDF形式でダウンロード (1060K) -
小出 隆規, 伊藤 ひろみ, 大高 章, 古谷 真優美, 北島 安雄, 藤井 信孝1993 年 41 巻 9 号 p. 1596-1600
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーα-Rat atrial natriuretic peptide (7-28) (rANP (7-28)) and a series of its analogs in which half cystine residue(s) were substituted with half selenocystine residue(s) were synthesized by using the Fmoc-based solid-phase method followed by cyclization by means of dimethylsulfoxide (DMSO)-trifluoroacetic acid (TFA) oxidation. These analogs possess comparable activities in both receptor binding and cGMP accumulation in rat vascular smooth muscle cells to those of rAMP (7-28).抄録全体を表示PDF形式でダウンロード (690K) -
川口 哲央, 山内 雄二, 前田 初男, 大森 秀信1993 年 41 巻 9 号 p. 1601-1603
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーEffects of ionic surfactants on the amperometric response of Fe(CN)3-6 at a gold electrode modified with the self-assembled monolayer (SAM) of an alkanethiol were examined in a flow system using an aqueous solution of a supporting electrolyte as the mobile phase. The response was enhanced by a cationic surfactant but depressed by an anionic surfactant, being detected as a positive and a negative peak, respectively. Octyl- and decylthiol were suited for the electrode modifier, and LiCl or NaCl was the electrolyte of choice. With 5% aqueous MeOH containing NaCl (0.1M) and K3Fe(CN)6 (5mM) as the mobile phase, the amperometric peak area was linearly correlated with the concentration of surfactants, indicating that the SAM-modified electrode is a prospect as a detector for surfactants in high-performance liquid chromatography.抄録全体を表示PDF形式でダウンロード (519K) -
香川 清水, 十倉 一也, 内田 清久, 嘉久志 寿人, 四家 勉, 菊池 純子, 中井 博, / , Loknath SUBEDI1993 年 41 巻 9 号 p. 1604-1607
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーThe 90% methanol-soluble fraction of a Bhutanese medicinal plant, Shug Chher, exhibited inhibition of platelet aggregation induced by platelet activating factor. Bioassay-directed fractionation led to the isolation of four new labdane diterpenoids, 3α, 15-dihydroxy-labda-8(17), 13E-diene (5), 3α-hydroxy-labda-8(17), 13E-dien-15-oic acid (6), 3α-hydroxy-labda-8(17), 12E, 14-trien-19-oic acid (7), and 3α-acetoxyisocupressic acid (8) and four known diterpenoids, manool (1), 3α-hydroxymanool (2), 3α-hydroxy-12, 13E-biformene (3), and isocupressic acid (4). The structures of the new compounds were determined spectroscopically. Compounds 2, 3, and 5 inhibited platelet aggregation.抄録全体を表示PDF形式でダウンロード (633K) -
縣 功, 日下部 聖, 波多野 力, 西部 三省, 奥田 拓男1993 年 41 巻 9 号 p. 1608-1611
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーTwo new polyphenolic compounds, melitric acids A (2) and B (5), were isolated from the aboveground part of Melissa officinalis (Labiatae) and their structures, consisting of three caffeic acid units, were determined from chemical rections and spectral data. Rosmarinic acid (1) was also isolated.抄録全体を表示PDF形式でダウンロード (646K) -
木島 孝夫, 高崎 みどり, 小塚 睦夫, 春名 光昌, 伊藤 一男, / , Kuo-Hsiung LEE1993 年 41 巻 9 号 p. 1612-1615
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーIn our search for possible anti-tumor-promoters, we carried out an investigation of the leaves and branches of Cowania mexicana D. DON (Rosaceae). Two new cucurbitane type triterpenes, 15-oxo-cucurbitacin F (3) and 15-oxo-23, 24-dihydrocucurbitacin F (4), were isolated together with cucurbitacin F (1) and 23, 24-dihydrocucurbitacin F (2). These triterpenes were inhibitors of Epstein-Barr virus early antigen activation induced by 12-O-tetradecanoylphorbol-13-acetate, a well-known tumor-promoter. The structures of 3 and 4 were determined from 2D-NMR spectral data and difference NOE experiments.抄録全体を表示PDF形式でダウンロード (607K) -
鈴木 正彦, 井東 喜代子, 伏見 千種, 近藤 保1993 年 41 巻 9 号 p. 1616-1620
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーThe interaction of sodium salicylate and naphazoline hydrochloride with polyvinylpyrrolidones having four different molecular weights (10, 25, 40, and 360kDa), and with the micelles of non-ionic surfactant polyoxyethylene n-dodecylethers having various numbers of oxyethylene units (5, 6, 7, and 8) were investigated using the freezing point depression method. The advantages of this method are that the binding parameters can be rapidly obtained by a simple procedure using a commercially available osmometer. Based on the colligative properties, the binding parameters were calculated. The data were expressed in the form of nonlinear Scatchard plots. The results suggested that salicylate and naphazoline were bound to two kinds of binding sites on a molecule of polyvinylpyrrolidone or to a micelle of polyoxyethylene n-dodecylether; the primary binding site exhibited a high affinity but a low capacity for the drug, while the second binding site has a lower affinity and a high capacity; that is, the interaction on the second binding site could be described as non-specific binding. For the interactions of drugs with polyvinylpyrrolidone, the number of N-vinyl-2-pyrrolidone units (monomer) that interacted with one molecule of salicylate and naphazoline were fairly constant, and from 10 to 14 and from 21 to 30, respectively. For the interactions of drugs with a micelle of polyoxyethylene n-dodecylether, the number of polyoxyethylene n-dodecylether molecules which interacted was also nearly constant at 3 to 4 and 5 to 6, respectively.抄録全体を表示PDF形式でダウンロード (750K) -
飯田 耕太郎, 大塚 昭信, 檀上 和美, 砂田 久一1993 年 41 巻 9 号 p. 1621-1625
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーIn order to study the effect of surface roughness and substrate material type on the adhesion of particles, measurements were made using the pendulum impact separation method using a variety of powders and substrates. Two methods were used to attach powder particles to a substrate : the free falling method and the fluidized method. When the powders were deposited on a substrate by free falling (with negligible force), the force of adhesion to the substrate with a rough surface was less than the adhesion to the smooth surface substrate. The degree of reduction in adhesive force increased as the shape of sample powder more closely resembled a sphere. When the powders were attached to a substrate under a fluidized state, a remarkable increase in adhesive force was observed in organic powder/polyvinyl chloride (PVC) systems. This is probady due to the electrostatic force produced by the collision and/or friction of particles to the PVC sheet.抄録全体を表示PDF形式でダウンロード (916K) -
石川 正直, 松野 陽子, 野口 章公, 葛谷 昌之1993 年 41 巻 9 号 p. 1626-1631
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA controlled-release tablet can be obtained by oxygen plasma irradiation on the outer layer double-compressed tablets prepared from theophylline as a core material and polycarbonate derived from bisphenol A (PC) as a single wall material, making this possible that PC is of intramolecular bifunctionality, crosslinkable phenyl group and degradable carbonate group as an effect of plasma irradiation. It was shown that the dissolution profiles can be varied so as to cause release of theophylline at different rates, depending on the set of conditions chosen for tablet manufacturing as well as plasma operational conditions.抄録全体を表示PDF形式でダウンロード (1509K) -
内田 武, 米持 悦生, 小口 敏夫, 寺田 勝英, 山本 恵司, 仲井 由宣1993 年 41 巻 9 号 p. 1632-1635
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーFour crystalline forms of tegafur were prepared by recrystallization from different solvents (α-, β-, δ-forms) and by heating (γ-form). They have been characterized using powder X-ray diffraction, thermal analysis, microscopy, density measurements and infrared spectroscopy. From differential scanning calorimetry measurements, it was confirmed that the γ- and δ-forms melted at 175°C and 165°C, whereas the α- and β-forms transformed into the γ-form at about 162°C and 120°C, respectively. The infrared absorption spectral differences observed between the α- and β-forms were discussed in relation to their intermolecular hydrogen bonding systems. It was also found that the difference in crystal forms significantly altered the dissolution rate of tegafur.抄録全体を表示PDF形式でダウンロード (1322K) -
福岡 英平, 寺田 勝英, 牧田 みどり, 山村 重雄1993 年 41 巻 9 号 p. 1636-1639
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA pattern-fitting procedure was described to determine the strength of preferred orientation of crystallite in tablets using X-ray powder diffraction data. This method is based on the pattern-fitting crystal structure refinement method which also uses powder diffraction data. Observed X-ray scattering intensities were fitted to analytic expression including some fitting parameters, namely peak positions, peak widths, background intensities and preferred orientation. All fitting parameters were optimized by non-linear least-squares procedure. Then the strength of preferred orientation of crystallites was evaluated from the magnitude of preferred orientation parameter.Aspirin was used for the sample, and though aspirin crystallites showed little preferred orientation in powders, they showed marked preference in tablets. The magnitude of preferred orientation parameter increased with increasing compression pressure of tablet. This indicated that aspirin crystallites showed stronger preferred orientation in tablets prepared under higher compression pressure.抄録全体を表示PDF形式でダウンロード (656K) -
木内 文之, 後藤 義久, 杉本 直樹, 赤尾 信明, 近藤 力王至, 津田 喜典1993 年 41 巻 9 号 p. 1640-1643
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA new curcuminoid, cyclocurcumin (IV), was isolated from the nematocidally active fraction of turmeric, the rhizome of Curcuma longa, together with three known curcuminoids, curcumin (I), demethoxycurcumin (II) and bisdemethoxycurcumin (III). The structure of IV was elucidated on the basis of spectral data and confirmed by the partial synthesis from curcumin (I). Although the above curcuminoids were ineffective when they were applied independently, the nematocidal activity increased remarkably when they were mixed, suggesting a synergistic action between them.抄録全体を表示PDF形式でダウンロード (644K) -
永田 和弘, 伊藤 喬, 岡田 真弥子, 大沢 昭緒1993 年 41 巻 9 号 p. 1644-1648
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーVicarious nucleophilic substitution using chloromethyl phenyl sulfone was applied to pyridinium and 1, 2, 3-triazinium dicyanomethylides to afford corresponding 4-substituted pyiridinium and 5-substituted triazinium dicyanomethylides, respectively. They were readily transformed to 4-phenylsulfonylmethylpyridines and 5-phenylsulfonylmethyltriazines by radical reaction.抄録全体を表示PDF形式でダウンロード (788K) -
棚橋 孝雄, 島田 厚子, 永倉 直敬, 井上 謙一郎, 桑島 博, 高石 清和, 陳 成章, 賀 震旦, 楊 崇仁1993 年 41 巻 9 号 p. 1649-1651
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA secoiridoid glucoside, insularoside-6‴ -O-β-D-glucoside, was isolated along with 9 known compounds from the leaves of Fraxinus insularis and its structure was determined to be 2 on the basis of spectroscopic and chemical studies. Direct comparison of this glucoside with a known secoiridoid glucoside, oleayunnanoside, led to the conclusion that the two were identical, and that the proposed structure 2a for oleayunnanoside should be revised to 2.抄録全体を表示PDF形式でダウンロード (570K) -
小川 知行, 末宗 洋, 酒井 浄1993 年 41 巻 9 号 p. 1652-1654
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA new method for diastereo- and enantioselective preparation of 1, 3-polymethyl functions was studied. The reaction of (1'R, 2'R, 5R)-(2E)-2'-hydroxycyclohexyl 5, 9-dimethyl-2, 8-decadienoate (6) with Me2 CuLi afforded a diastereomeric mixture of conjugate addition products ((3R, 5R)-9 and (3S, 5R)-9) in a ratio of 77 to 23.抄録全体を表示PDF形式でダウンロード (537K) -
石井 永, 小林 純一, 山口 啓一, 石川 勉1993 年 41 巻 9 号 p. 1655-1656
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーThe X-ray structure of toddalosin (1), a new biscoumarin, isolated from Toddalia asiatica (L.) LAM. (T. aculeata PERS.) is described.抄録全体を表示PDF形式でダウンロード (397K) -
井藤 千裕, 中川 真由美, 井上 真美, 竹村 優子, 十一 元晴, 大村 三男, 古川 宏1993 年 41 巻 9 号 p. 1657-1658
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーA new dimeric coumarin (biscoumarin) named bisparasin (1) was isolated from some hybrid plants of Citrus species. On the basis of spectrometric analyses, the structure was characterized as a [2+4] cycloaddition adduct between trans-dehydroosthol (2) and citrubuntin (3).抄録全体を表示PDF形式でダウンロード (426K) -
久保寺 登, 渡邉 博義, 宮本 勝仁, 松本 雅彦, 松岡 雪, 河西 武彦1993 年 41 巻 9 号 p. 1659-1663
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーFour vitamin D3 analogues, 1α, 24(S)-and 1α, 24(R)-dihydroxy-22-oxavitamin D3 (5 and 6) and their 20(R)-epimers (7 and 8) were synthesized from the 20(S)-alcohol (10). In tests of activity to induce differentiation of human myeloid leukemia cells (HL-60) to macrophages, 5 showed comparable activity to 1α, 25-dihydroxy-22-oxavitamin D3 (OCT) (2), and the other three analogues (6, 7 and 8) were less active than OCT (2). The binding properties of these analogues to the chick embryonic intestinal 1α, 25-dihydroxyvitamin D3 (1) receptor were evaluated. Furthermore, 20(R)-OCT (9) was synthesized and its biological properties were compared with those of OCT (2) and the 20(R)-epimers (7 and 8).抄録全体を表示PDF形式でダウンロード (729K) -
白橋 秀明, 村上 啓寿, 渡邊 美也子, 永津 明人, 榊原 仁作, 徳田 春邦, 西野 輔翼, 岩島 昭夫1993 年 41 巻 9 号 p. 1664-1666
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーBioassay-directed fractionation of the extract of the cyanobacterium P. tenue led to the isolation of the three classes of glycolipids, viz., monogalactosyl diacylglycerol (MGDG), digalactosyl diacylglycerol (DGDG), and sulfo-quinovosyl diacylglycerol (SQDG) as anti-tumor-promoters. In comparing the anti-tumor-promoting effect of the three classes of glycolipids with various acyl residues, MGDG and DGDG inhibited tumor promotion more intensely than SQDG. With respect to MGDG and DGDG, the inhibitory activity of each glycolipid possessing a single pair of acyl residues was also investigated after HPLC separation. Among the 17 tested MGDGs (1a-h) and DGDGs (2a-i), three of the DGDGs (2a, b, e) showed more potent inhibitory activity toward tumor promotion than the others.抄録全体を表示PDF形式でダウンロード (575K) -
北島 潤一, 田中 靖子1993 年 41 巻 9 号 p. 1667-1669
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーFrom the methanol extract of the crude drug "She chuang zi" [Japanese name "Jyashoshi", the fruit of Cnidium monnieri CUSSON (Umbelliferae)], two new substances were obtained as the main constituents of the water soluble portion. From the results of spectral investigations, they were characterized as 3, 7-dimethyl-1, 2, 6, 7-tetrahydroxyoct-3(10)-ene (obtained as a mixture of two epimers) and 3-methyl-1, 2, 3, 4-tetrahydroxy-butane, respectively. It is interesting that such monoterpenoid and hemiterpenoid tetraols were obtained from the water soluble portion of an Umbelliferous crude drug which contained an abundance of essential oil and coumarin derivatives.抄録全体を表示PDF形式でダウンロード (499K) -
奥山 恵美, 中村 智徳, 山崎 幹夫1993 年 41 巻 9 号 p. 1670-1671
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーConvulsants veranisatin A and B, isolated from Star Anise (Illicium verum Hook.f.), were structurally elucidated by spectroscopic data and compared with anisatin-related compounds.抄録全体を表示PDF形式でダウンロード (400K) -
李 波, 田中 圭, 冨士 薫, 孫 漢董, 多賀 徹1993 年 41 巻 9 号 p. 1672-1673
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーThe structures of taxchinins D and G and taxchin A have been determined by means of NMR spectroscopy and confirmed by X-ray analyses. The fomer two possess a rearranged taxane skeleton found in taxchinin A, while the latter has a taxane skeleton.抄録全体を表示PDF形式でダウンロード (377K) -
横山 祥子, 春原 政明, 藤江 忠雄1993 年 41 巻 9 号 p. 1674-1676
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーThe release of nicotinamide (NAA) from docosanoic acid (C22)-NAA complex was measured in pH 1.2-6.8 aqueous media. The release of NAA was ON-state below pH 6.2 and OFF-state at pH 6.8, suggesting that the release behavior is applicable to a pH-responsive drug delivery system.抄録全体を表示PDF形式でダウンロード (381K) -
吉川 雅之, 山口(旧姓 畠山) 祥子, 村上 敏之, 松田 久司, 山原 條二, 村上 啓寿1993 年 41 巻 9 号 p. 1677-1679
発行日: 1993/09/15
公開日: 2008/03/31
ジャーナル フリーFour new biologically active diterpenes, trifoliones A, B, C, and D, were isolated from the tuber of Sagittaria trifolia L. together with three new glycosides, sagittariosides a and b and arabinothalictoside. Their stereostructures were determined on the basis of chemical and physicochemical evidence which included the application of a modified Mosher's method and an exciton chirality method. Trifoliones A, B, C, and D exhibited inhibitory effects on the histamine release from rat mast cells induced by compound 48/80 or calcium ionophore A-23187.抄録全体を表示PDF形式でダウンロード (595K)
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